33 results about "Valsartan" patented technology

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from aspirin, atorvastatin, valsartan, hydrochlorothiazide, folic acid substances and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition provided by the invention has the advantages that the pharmaceutical composition provided by the invention has a multi-target synergistic prevention effect on vascular diseases, especially cerebral embolism, that is, the composition not only can reduce blood pressure, blood fat and blood homocysteine level, but also has an effect of preventing thrombosis, and reduces the risk of cerebral apoplexy. In addition, the form of the pharmaceutical composition is beneficial to improving the medication compliance of patients.

The invention discloses a valsartan-silicon dioxide micro-capsule orally disintegrating tablet and a preparation method thereof, and relates to the technical field of medicines. The invention relates to a preparation method of a valsartan-silicon dioxide micro-capsule orally disintegrating tablet. The preparation method comprises the following steps: S11, preparing an aqueous solution of a cationic surface active agent; s12, valsartan is added and stirred, so that the surface of valsartan is positively charged; s13, continuing to add silicon dioxide and stirring to enable a silicon dioxide monomer to be adsorbed on the surface of valsartan; and S14, continuously adding the cationic polymer and carrying out high-speed shearing, so that the cationic polymer is encapsulated on the surface of the silicon dioxide. The valsartan-silicon dioxide micro-capsule orally disintegrating tablet prepared by the invention has a medicine taste masking effect, and the taste masking effect is excellent; meanwhile, the problems of poor compressibility and flowability of materials caused by hygroscopicity and viscosity of valsartan are solved; a sweetening agent and a flavoring agent are not needed in the formula, so that the formula is simplified, impurities are prevented from being introduced into the essence, and the stability is effectively improved.

The invention belongs to the technical field of pharmaceutical chemistry and natural product separation, and provides application of tribulus terrestris polysaccharide. The tribulus terrestris polysaccharide can be used for preparing drugs for treating hypertension. The tribulus terrestris polysaccharide has the effects of reducing blood pressure, relieving vascular endothelium pathological injury, improving vascular endothelium dysfunction and protecting vascular endothelium on a hypertensive rat model. The treatment effect of the fried tribulus terrestris polysaccharide is obviously superior to that of the tribulus terrestris polysaccharide, and meanwhile, the blood pressure reducing effect of the fried tribulus terrestris polysaccharide is not obviously different from that of a positive medicine valsartan. A new material basis is provided for development of antihypertensive drugs, and meanwhile the medicinal value of the tribulus terrestris polysaccharide is expanded.

Disclosed herein is a process for the preparation and purification of Valsartan. The process according to the invention is capable of removing the toxic nitroamine impurities and providing substantially pure Valsartan.

The present application relates to a kind of valsartan-2-amino pyridine co-amorphous and preparation method, the co-amorphous of valsartan-2-amino pyridine of the present application is with 2-amino pyridine according to specific proportion mixed, using solvent evaporation method to prepare single-phase amorphous binary system, the present application uses the interaction between 2-amino pyridine and valsartan, forms ternary hydrogen bond connection mode, greatly improves the solubility and dissolution of valsartan, improves bioavailability, and cost is low, energy consumption is low, can large-scale industrial production.

The application belongs to the technical field of medicine synthesis, and particularly relates to a synthesis and refining method of valsartan. After L-valseril is used to prepare a crude valsartan product, ultrasonic-assisted crystallization is used to obtain high-purity valsartan. The synthesis and refining method significantly reduces the content of D-isomer, avoids multiple purification treatment steps, is simple in process and easy to operate, and provides a method for recovering L-valseril from a valsartan mother liquor, so as to further improve the utilization rate, reduce the cost, and be suitable for industrial production.

The utility model provides a parallel micro-channel reaction system which comprises a feeding pump A, a feeding pump B, an ultrasonic flowmeter A, an ultrasonic flowmeter B, a check valve, a feeding pipe A, a feeding pipe B, a micro-channel reactor A, a micro-channel reactor B, a high-low temperature integrated circulator, a discharging pipe A, a discharging pipe B, a combined pipeline and a reaction tank, the high-low temperature integrated circulator is connected with the micro-channel reactor A and the micro-channel reactor B through a circulating freezing liquid pipe A and a circulating freezing liquid pipe B, and the reaction tank is used for containing a reaction solution. The parallel micro-channel reaction system not only improves the yield of the sacubitril valsartan sodium intermediate, but also fills the technical blank that the micro-channel reactors are not used in commercial mass production in the market and no double-plate parallel micro-channel reactor exists, is suitable for capacity expansion of all micro-channel reactors, and has no amplification effect.

This invention belongs to the field of pharmaceutical technology, and specifically relates to a vildagliptin-valsartan co-amorphous compound, its preparation method, and its application. The co-amorphous compound comprises vildagliptin and valsartan; the molar ratio of vildagliptin to valsartan in the co-amorphous compound is 1:0.5-3. In this invention, vildagliptin and valsartan interact to form hydrogen bonds. This interaction not only prevents solvent-mediated drug recrystallization but also accelerates the dissolution and exudation of valsartan. Compared to the valsartan raw material, the solubility and dissolution rate of valsartan in this co-amorphous compound are significantly improved, while the solubility and dissolution rate of vildagliptin are reduced. This is beneficial for improving the bioavailability of valsartan, delaying the release and absorption of vildagliptin in vivo, and the co-amorphous compound exhibits good stability.

At least one pharmaceutical composition for use in a method of prophylaxis or treatment of COVID wherein the at least one pharmaceutical composition comprises donepezil, rivastigmine or galantamine or one of donepezil, rivastigmine or galantamine combined with one of: Artemether and Lumefantrine; Atazanavir Sulfate; Efavirenz; Fosamprenavir Calcium; Saquinavir; Remdesivir (GS-5734); Digoxin; Memantine; Rivastigmine; Galantamine; Valsartan; Teriflunomide and wherein the method of prophylaxis or treatment of COVID or COVID-19 comprises: providing a subject in need of said prophylaxis or treatment; providing the at least one pharmaceutical composition as defined supra; wherein said components are provided together or separately; wherein said components are administered together or separately; and wherein said components are provided in a pharmaceutically acceptable diluent, adjuvant and / or excipient; and administering a pharmaceutically effective amount of said at least one pharmaceutical composition to said subject; and wherein, in the method, said subject is provided prophylaxis or treatment of COVID and COVID relates to a human coronavirus, mouse hepatitis virus (MHV), or recombinant mouse-adapted SARS-CoV (SARS-CoV MAI 5).

The invention discloses a practical synthesis method of a chiral ligand S, Sp-tBu-FOXAP (S, Sp-tBu-FOXAP). By improving the synthesis process in the literature, the production operation is simpler. Compared with a column chromatography purification mode used in each step in the literature, the novel process does not need column chromatography purification, the product can be purified through pulping or recrystallization, the purity of the final product can reach 97.0% or above, the ee value is larger than 99.0%, the d.r. Value is larger than 20: 1, purification is simple, and the cost is greatly reduced. The chiral ligand prepared by the new process can be used as a catalyst for asymmetric hydrogenation reaction after in-situ complexation with ruthenium metal, and can be used for catalytic synthesis of a key intermediate of savobabatrivalsartan which is a savobabatrivalsartan which is a marketable medicine.

The invention belongs to the field of pharmaceutical synthesis technology, and in particular to a method for synthesizing a valsartan intermediate. This method uses 4'-hydroxymethyl-2-cyanobiphenyl as a raw material and reacts with L-valine methyl ester hydrochloride under the action of a catalyst. Finally, the target product is obtained by concentration, salification, and drying. The target product obtained by this method has a higher yield and purity, and can effectively avoid the generation of dimer impurities in the prior art, has simple post-processing, and is suitable for industrial production.

The invention belongs to the technical field of biological medicines, and particularly relates to application of an angiotensin II receptor antagonist in preparation of a medicine for preventing and treating renal tubular injury caused by triptolide. According to the invention, the upstream key target protein of the TPL-induced renal tubule injury is determined to be HSPA1 through experiments for the first time, and the problem that the key target spot of TPL toxicity is not determined in the prior art is solved. Based on a key target spot of TPL toxicity, through molecular screening and parallel pharmacodynamic verification on various sartan drugs such as irbesartan, losartan, olmesartan and valsartan, it is determined that the angiotensin II receptor antagonist has a general protection effect on TPL toxicity. Wherein the protective efficacy of irbesartan as a preferable embodiment is obviously superior to that of losartan of the same kind (the efficiency slope is 2.451 to 1.584).

The invention provides a means for prevention and adjuvant therapy of pulmonary vein stenosis, and particularly provides application of valsartan in preparation of drugs for prevention and adjuvant therapy of pulmonary vein stenosis. The valsartan can slow down the progress of intimal hyperplasia by inhibiting TGF-beta related pathways, so that the probability of occurrence of pulmonary vein stenosis is reduced. Therefore, the fusion protein can be used as an auxiliary treatment for surgical intervention, especially for preventing or treating acquired pulmonary vein stenosis after a complete pulmonary vein abnormal junction operation of children, and can reduce the occurrence probability of the acquired pulmonary vein stenosis after the operation and improve prognosis.

The invention belongs to the technical field of pharmaceutical analysis, and particularly provides a method for detecting the content of potassium ions in Milsartan potassium, which comprises the following steps: S1, preparing a potassium ion reference solution and a Milsartan potassium test solution; s2, respectively detecting the reference substance and the test sample by adopting HPLC-CAD (High Performance Liquid Chromatography-Computer Aided Design), recording a chromatogram, and calculating the content of potassium ions; wherein the conditions of the high performance liquid chromatography are as follows: a mixed mechanism chromatographic column is adopted, an ammonium formate aqueous solution is used as a mobile phase A, acetonitrile is used as a mobile phase B, and isocratic elution is performed. According to the method for detecting the content of the potassium ions in the Milsartan potassium, provided by the invention, the potassium ions in the Milsartan potassium are controlled by adopting an external standard method according to the characteristics of the Milsartan potassium. The method is accurate, reliable, high in sensitivity and good in repeatability, can rapidly and efficiently measure the content of the potassium ions in the Milsartan potassium, provides an effective technical means and data support for subsequent Milsartan potassium content detection, and can be used for evaluating the quality of Milsartan potassium drugs.

The invention discloses valsartan production ingredient adding equipment and an ingredient adding method.The valsartan production ingredient adding equipment comprises an infiltration mechanism, an auxiliary mechanism, a cover plate and a feeding pipe, atomization nozzles are annularly and evenly distributed in an infiltration ring, and therefore water mist in an infiltration tank body and a mechanism tank body is distributed more evenly; the material distributing baffle can scatter powder entering the infiltrating tank body and the mechanism tank body, meanwhile, the material distributing baffle is matched with the powder raising fan to raise the distributed materials in the mechanism tank body and the infiltrating tank body, and the powder flying in the infiltrating tank body is combined with water mist in the infiltrating tank body, so that the infiltrating effect on the powder is improved; the infiltrating rings and the inner walls of the infiltrating tanks on the two sides are in smooth transition to form inclined planes, and water mist can smoothly flow along with the surfaces of the infiltrating rings, the surfaces of the inner walls of the infiltrating tanks and the inclined planes between the infiltrating rings and the infiltrating tanks after being condensed on the surfaces of the infiltrating rings and the surfaces of the infiltrating tanks. Flying dust and water mist in the infiltrating tank body can be effectively prevented from caking on the surface of the infiltrating tank body.

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from amlodipine with the minimum hypertension treatment dosage of 20%-50%, valsartan with the minimum hypertension treatment dosage of 20%-50%, metoprolol with the minimum hypertension treatment dosage of 20%-50%, hydrochlorothiazide with the minimum hypertension treatment dosage of 20%-50%, homocysteine reducing medicine and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition is used for treating hypertension, is especially suitable for hypertension with heart failure, and can reduce the death risk of patients.

The invention discloses a supramolecular group composite peptide-containing antihypertensive composition, which is composed of raw materials and basic energy substrates, the raw materials comprise composite peptide, phytosterol, taurine and the like, and the basic energy substrates comprise proteins, dietary fibers, fatty acids and / or lipids; the composite peptide is composed of Anbenefit milk polypeptide and balsam pear peptide. According to the present invention, the components of the specific types and the specific amounts are selected and compounded, such that the prepared composition has effects of significant cardiac output reducing and blood vessel diameter increasing, and the partial composition can cooperate with valsartan (antihypertensive drug) to achieve effects of synergistic blood pressure reducing so as to provide effects of auxiliary improvement or prevention of blood pressure reducing. Therefore, the method can be used for developing functional foods and medicines and has a considerable market prospect.

The present invention relates to compositions, systems, and methods for treating a subject with an eye condition (e.g., topically) using a composition comprising an ACE-2 receptor antagonist (also known as Angiotensin II Receptor Blocker or “ARB”) (e.g., losartan, telmisartan, valsartan, olmesartan, candesartan, irbesartan, eprosartan, azilsartan, or losartan metabolite EXP3174). In certain embodiments, the eye condition is selected from: i) a corneal scarring fibrosis, ii) a transforming growth factor beta-induced (TGFBI) corneal dystrophy, iii) a conjunctival fibrotic disease, iv) an intraocular fibrotic disease, and v) a conjunctival bleb scarring and / or shunt encapsulation (e.g., following glaucoma surgery).

The application discloses a valsartan impurity (5-(4'-(chloromethyl)-[1,1'-biphenyl]-2-yl)-1H-tetrazole) and a preparation method thereof. The structure of the valsartan impurity is shown as formula I. The preparation method takes compound 5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole as a starting material, reacts with hydrochloric acid in a solvent, and obtains the valsartan impurity shown as formula I. The valsartan impurity has the advantages of mild reaction condition, simple process, short reaction time, good yield, high-purity 5-(4'-(chloromethyl)-[1,1'-biphenyl]-2-yl)-1H-tetrazole, reliable impurity control sample for quality control research of a valsartan product, and great significance.

The invention discloses a method for separating and detecting enantiomers in a valsartan amlodipine pharmaceutical composition, and belongs to the field of pharmaceutical analysis. The method uses a reversed-phase chromatographic column with C18 as a filler, uses acetonitrile-water containing triethanolamine as a mobile phase, and utilizes isocratic elution to carry out HPLC separation and determination of the valsartan enantiomers in the valsartan amlodipine pharmaceutical composition. The reversed-phase chromatography system used in the present invention has the advantages of stable chromatographic medium performance, wide pH tolerance range, strong separating power, easy operation, etc., and the inventive method has good specificity, good accuracy, low requirements for instrumentation, good sensitivity, good injection precision and repeatability, good actual detection effect, and can better control the product quality of the valsartan amlodipine pharmaceutical composition.

The invention discloses an oral solid preparation of valsartan. The oral solid preparation comprises a valsartan eutectic compound and pharmaceutically acceptable auxiliary materials, the oral solid preparation comprises tablets, capsules and granules, and the content of the active substance valsartan is 10-320 mg. The valsartan eutectic compound is prepared by forming a supramolecular compound from valsartan and a specific eutectic precursor molecule (such as nicotinamide), loading the supramolecular compound in a pore channel of a mesoporous silica nano-carrier with a high specific surface area in a confinement manner, and modifying the supramolecular compound with a surface stabilizer. According to the method, medicine crystallization is inhibited by utilizing a nano confinement effect, and the medicine exists in an amorphous or molecular-level dispersed high-energy state under the synergistic action of eutectic precursor molecules, so that the dissolution rate and oral absorption efficiency of the medicine are greatly improved. The valsartan preparation is simple in process, good in stability and suitable for industrial production, and the prepared valsartan preparation has excellent in-vitro dissolution rate and in-vivo bioavailability.

The invention discloses a compound shown in a formula (I) and a preparation method thereof. The compound is used as a reference substance of a novel potential process impurity in quality control of sartan antihypertensive drugs with biphenyl tetrazole structures, such as olmesartan medoxomil, allisartan medoxomil, losartan, candesartan cilexetil, ibesartan, valsartan and the like. # imgabs0 #

The invention discloses a composition containing valsartan and fineglitazone and a preparation method of the composition, and relates to the technical field of pharmaceutical compositions.According to the composition, valsartan, fineglitazone, a curcumin phospholipid complex and L-arginine are scientifically proportioned, a three-dimensional kidney protection network is constructed, and the kidney protection effect is improved. Valsartan and fineglitazone cooperate to block excessive activation of RAAS, blood pressure is effectively reduced, glomerular hyperfiltration is relieved, aldosterone-mediated renal fibrosis and inflammatory response can be inhibited, on the basis, the curcumin phospholipid complex improves bioavailability of fat-soluble curcumin through a phospholipid carrier, and the bioavailability of fat-soluble curcumin is improved. The microencapsulated L-arginine can specifically enhance the activity of antioxidant enzymes in kidney tissues and relieve oxidative damage to renal tubular epithelial cells, and the microencapsulated L-arginine serves as an NO precursor substance, controls the slow release rate through an eudragit EPO coating, continuously supplements an NO synthetic substrate, repairs an NO signal channel of damaged vascular endothelial cells and reduces serum creatinine and urea nitrogen levels.

The method for detecting the triphenylphosphine oxide in the sacubitril valsartan sodium starting material is established by adopting a high performance liquid chromatography method. Through verification, the detection method has the advantages of high sensitivity, strong specificity, high accuracy, durability and reliability, and can realize effective control of triphenylphosphine oxide in sacubitril-valsartan sodium, thereby ensuring the medicine quality of sacubitril-valsartan sodium and the effectiveness and safety of patient medication.

The present invention discloses a new use of salvianolic acid B. The present invention uses an experiment on a lung cancer heart disease model constructed with urethane and benzopyrene to determine that salvianolic acid B, Panax notoginseng total saponins, especially salvianolic acid B combined with Panax notoginseng total saponins, can improve the heart function of mice with lung cancer heart disease by increasing the left ventricular ejection fraction and the left ventricular short axis shortening rate, reducing the left ventricular end-systolic diameter and left cardiac output, and reducing the right heart free wall thickness, right heart end-diastolic diameter, right ventricular stroke volume and right cardiac output. While many drugs for treating heart-related diseases have poor effects on the heart function of lung cancer heart disease, the effect of salvianolic acid B combined with Panax notoginseng total saponins on improving heart function is comparable to that of sacubitril-valsartan, which is currently commonly used in clinical practice, and has achieved unexpected therapeutic effects, with broad application prospects.

The invention provides a preparation method of valsartan granules, and belongs to the field of pharmaceutical preparations. Dynamic gradient control is carried out on the air inlet temperature, and the atomization pressure and the liquid spraying amount are adjusted to be cooperatively matched with the air inlet temperature, so that dynamic balance of the temperature increasing speed, the liquid drop size and the particle growth rate is guaranteed, the phenomenon of particle surface overmelting or wet nucleus aggregation is avoided, generation of too thick or too fine particles is eliminated, and the particle size is increased. The consistency of particle size growth dynamics is ensured, and the product quality stability is improved.

The present invention discloses a valsartan-silica microcapsule orally disintegrating tablet and a preparation method thereof, relating to the technical field of medicine. A preparation method of a valsartan-silica microcapsule orally disintegrating tablet comprises the following steps: S11: preparing an aqueous solution of a cationic surfactant; S12: adding valsartan and stirring to make the surface of valsartan carry a positive charge; S13: continuously adding silica and stirring to make silica monomers adsorb on the surface of valsartan; S14: continuously adding a cationic polymer and performing high-speed shearing to make the cationic polymer encapsulate on the surface of silica. The valsartan-silica microcapsule orally disintegrating tablet prepared by the present invention has a drug taste masking effect, and the taste masking effect is excellent; at the same time, it overcomes the problems of poor compressibility and fluidity of materials caused by the hygroscopicity and viscosity of valsartan; since no sweeteners and flavoring agents are required in the formula, the formula is simplified, the introduction of impurities by flavors is avoided, and the stability is effectively improved.

A compound comprising of the angiotensin receptor antagonist (ARB) valsartan, the neutral endopeptidase inhibitor (NEPi) (2R,4S)-5-biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methylpentanoic acid ethyl ester and one or more monovalent cations such as Nat useful for the treatment of hypertension and / or heart failure.

The invention relates to a pharmaceutical composition for treating hypertension and a preparation method thereof, in particular to a pharmaceutical composition containing valsartan and levamlodipine besylate. The valsartan and the levamlodipine besylate are combined for use, so that the valsartan and the levamlodipine besylate not only can play a synergistic effect and enhance a treatment effect, but also have relatively high safety and relatively low adverse reaction occurrence rate, and are worthy of wide popularization and application. By controlling the crystal form of levamlodipine besylate and the particle sizes of valsartan, levamlodipine besylate, filler, disintegrating agent, lubricant and glidant and packaging with medicinal aluminum foil, polyvinyl chloride solid medicinal hard tablets and polyamide / aluminum cold-formed solid medicinal composite hard tablets, the dissolution rate and stability of the medicine are optimized. According to the method, direct powder tabletting is adopted, the powder fluidity is good, tabletting is easy, the production time is shortened, the production efficiency is improved, and the product stability is also improved. In-vitro dissolution experiments show that the dissolution curve of the composition is consistent with that of a control preparation, and the composition has good bioavailability.

The present invention discloses a method for preparing and purifying valsartan. The method of the present invention can remove toxic nitrosamine impurities and provide substantially pure valsartan.